| 货号 | 9000491-50mg |
| 描述 | SR 144528 is a selective peripheral cannabinoid (CB2) receptor inverse agonist that displays a Ki value of 0.6 nM for rat spleen and human recombinant CB2 receptors and a Ki value of 400 nM for rat brain and human recombinant CB1receptors.1,2 SR 144528 antagonizes the inhibitory effects of CP 55,940 on forskolin-induced adenylyl cyclase activity in CHO cells expressing hCB2(IC50 = 10 nM) but not in cells expressing hCB1(IC50 >10 µM).1 SR 144528 has been used to investigate the contribution of the CB2 receptor in the control of pain initiation as well as suppression of inflammation and immune activation.3,4,5,6 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Rinaldi-Carmona, M.,Barth, F.,Millan, J., et al. SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor. Journal of Pharmacology and Experimental Therapeutics 284(2), 644-650 (1998). 2.Portier, M.,Rinaldi-Carmona, M.,Pecceu, F., et al. SR 144528, an antagonist for the peripheral cannabinoid receptor that behaves as an inverse agonist. Journal of Pharmacology and Experimental Therapeutics 288(2), 582-589 (1999). 3.Barth, F., and Rinaldi-Carmona, M. The development of cannabinoid antagonists. Current Medicinal Chemistry 6, 745-755 (1999). 4.Di Marzo, V. Targeting the endocannabinoid system: To enhance or reduce? Nature Reviews.Drug Discovery 7, 438-455 (2008). 5.Iwamura, H.,Suzuki, H.,Ueda, Y., et al. In vitro and in vivo pharmacological characterization of JTE-907, a novel selection ligand for cannabinoid CB2 receptor. Journal of Pharmacology and Experimental Therapeutics 296(2), 420-425 (2001). 6.Wright, K.L.,Duncan, M., and Sharkey, K.A. Cannabinoid CB2 receptors in the gastrointestinal tract: A regulatory system in states of inflammation. British Journal of Pharmacology 153, 263-270 (2008). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 475.2 |
| 分子式 | C29H34ClN3O |
| CAS号 | 192703-06-3 |
| 稳定性 | ≥ 2 years |
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